70090-68-5Relevant academic research and scientific papers
Harnessing the Power of Catalysis for the Synthesis of CRTH2 Antagonist MK-1029
Cai, Chaoxian,Humphrey, Guy R.,Kosjek, Birgit,Pan, Jun,Ruck, Rebecca T.,Strotman, Neil A.,Vaswani, Rishi G.
, (2021/07/01)
The synthetic strategy utilized to prepare clinical supplies of CRTH2 antagonist MK-1029 is described. Specifically, the approach communicated is predicated on the intervention of five distinct catalytic methods, using three separate metals and an enzyme, to enable successful construction of this complex active pharmaceutical ingredient.
Compound of dipyrrolopyridine structure Preparation method and medical application
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, (2021/08/25)
The invention discloses a compound with a dipyrrolo-pyridine structure as well as a preparation method and medical application thereof. The compound provided by the invention has obvious inhibitory activity on JAK family proteins, is an effective JAK inhibitor, and has the prospect of being developed into drugs for inhibiting JAK and further treating diseases.
Biarylphosphonite gold(I) complexes as superior catalysts for oxidative cyclization of propynyl arenes into indan-2-ones
Henrion, Guilhem,Chavas, Thomas E. J.,Le Goff, Xavier,Gagosz, Fabien
supporting information, p. 6277 - 6282 (2013/07/11)
Striking gold: A series of variously functionalized propynyl arenes was smoothly converted into indan-2-ones by a new gold(I)-catalyzed oxidative cyclization process. [LAu]NTf2 (Tf=trifluoromethanesulfonyl) is a superior catalyst both in terms of yield and kinetics for the present transformation. Copyright
Synthesis of allenes via Nickel-catalyzed cross-coupling reaction of propargylic bromides with grignard reagents
Li, Qinghan,Gau, Hanmou
experimental part, p. 747 - 750 (2012/06/29)
We describe a convenient method for the synthesis of terminal allenes from cross-coupling of propargylic bromide with Grignard reagent. The reaction of propargylic bromide with 1.2 equivalents of Grignard reagent mediated by Ni(acac)2 (2 mol%) and Ph3P (4 mol%) in THF may produce terminal allenes in good yields and high regioselectivities at room temperature. Georg Thieme Verlag Stuttgart · New York.
SUBSTITUTED PHENOXYMETHYL DIHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
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, (2011/04/19)
The present invention relates to a series of substituted phenoxymethyl dihydro oxazolopyrimidinones of formula (I) defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invent
INDOLE DERIVATIVES AS CRTH2 RECEPTOR ANTAGONISTS
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Page/Page column 28, (2010/09/17)
Compound of formula (I) are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
2-CYANOPYRROLOPYRIMIDINES AND PHARMACEUTICAL USES THEREOF
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Page/Page column 35, (2010/02/08)
The invention relates to pyrrolo pyrimidines of formula (I), wherein Y represents -(CH2)t-O- or -(CH2)r-S-, p is 1 or 2, r is 1, 2 or 3, t is 1, 2 or 3, or Y is -(CH2)j- or -CH=CH-, j is 1 or 2; p is 1 or 2, or Y is -(CH2)f-, f is 1 or 2, p is 1, and the further radicals and symbols have the meaning as defined herein; their preparation, their use as pharmaceuticals, pharmaceutical compositions containing them, the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment of neuropathic pain and to a method for the treatment of such a disease in animals, especially in humans.
Alkynylated fused ring pyrimidine compounds
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, (2008/06/13)
A compound selected from those of formula (I): wherein W1 represents O, S, or —NR3 in which R3 represents hydrogen, alkyl, OH or CN; W2 represents a group selected from hydrogen, CF3, NH2,
Conversion of alkyl- and arylallenes into 1-alkynes through metallated intermediates
Taherirastgar,Brandsma
, p. 4035 - 4040 (2007/10/03)
A number of acetylenes RCH2C≡CH have been obtained by metallation of the allenes RCH=C=CH2 or mixtures of acetylenes and allenes with n-BuLi in THF-hexane and hydrolysis after allowing the metallated allenes to rearrange at roam temperature or by heating under reflux.
A NOVEL AND EFFICIENT METHOD TO PREPARE 3-(HETERO)ARYL-1-PROPYNES AND ITS APPLICATION TO THE STEREOSELECTIVE SYNTHESIS OF (2E,4E)-N-(2-METHYLPROPYL)-6-(2-METHYLPROPYL)-6-(2-THIENYL)-2,4-HEXADIENAMIDE, PIPEROVATINE AND (E)-N-(2-METHYLPROPYL)-6-(4-METHOXYPHENYL)-4-HEXYN-2-ENAMIDE
Rossi, Renzo,Carpita, Adriano,Lippolis, Vito,Benetti, Massimo
, p. 783 - 791 (2007/10/02)
Chemically pure 3-(hetero)aryl-1-propynes, 13, have been prepared in high overall yields by a novel method which involves: (a) a copper(I)-mediated cross-coupling between a halomethyl(hetero)arene, 16, and trimethylsilylethylmagnesium bromide, 17, to give a trimethylsilyl-3-(hetero)aryl-1-propyne, 18; (b) removal of the trimethylsilyl group from 18 by treatment with potassium fluoride dihydrate in DMF.One of these 1-alkynes, i.e. 3-(2-thienyl)-1-propyne, 13a, has been employed in the key step of a highly stereoselective synthesis of naturally-occurring (2E,4E)-N-(2-methylpropyl)-6-(2-thienyl)-2,4-hexadienamide, 6.On the other hand, 3-(4-methoxyphenyl)-1-propyne, 13b, has been used either in two stereoselective syntheses of another natural N-(2-methylpropyl) amide, i.e. piperovatine, 7, or in the preparation of a structural analogue of 7, i.e. (E)-N-(2-methylpropyl)-6-(4-methoxyphenyl)-4-hexyn-2-enamide, 15.
